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Life Sci ; 92(3): 237-44, 2013 Feb 27.
Artículo en Inglés | MEDLINE | ID: mdl-23295958

RESUMEN

AIMS: The current study describes the synthesis and pharmacological evaluation of (E)-N-(3,7-dimethylocta-2,6-dienyl)-1,3-dimethyl-1H-pyrazol-5-amine (LQFM002), a compound originally designed through a molecular simplification strategy from 4-nerolidylcatechol. LQFM002 was evaluated for preservation of the PLA(2) enzyme inhibitory effects of the lead compound, 4-nerolidylcatechol, using in vitro and in vivo models. MAIN METHODS: Rota-rod, open field and pentobarbital-induced sleeping tests were used to evaluate the effects of LQFM002 on the central nervous system. A gel plate assay of PLA(2) activity, carrageenan-induced pleurisy and TNF-α levels was used to assay anti-inflammatory activity. Antinociceptive activities of LQFM002 were evaluated with acetic acid-induced writhing, formalin and hot-plate tests, while involvement of the opioid pathway in the LQFM002 antinociceptive effect was investigated with naloxone pre-treatment. KEY FINDINGS: LQFM002 inhibited PLA(2) activity, cell migration into the pleural cavity, and capillary permeability (Evan's blue concentration) and reduced TNF-α levels in pleural exudates. LQFM002 also reduced acetic acid-induced writhing and the licking time in both phases of the formalin test and increased latency in the hot-plate test. Pre-treatment with 8.25 µmol/kg naloxone (3mg/kg) reversed the analgesic effects of LQFM002 in the early phase of the formalin test. SIGNIFICANCE: LQFM002 showed anti-inflammatory activity, which possibly involved reduction of leukocyte migration and TNF-α levels. LQFM002 also demonstrated inhibition of PLA(2) activity in vitro. LQFM002 had an antinociceptive effect that involved the opioidergic system.


Asunto(s)
Analgésicos/farmacología , Antiinflamatorios/farmacología , Catecoles/farmacología , Pleuresia/tratamiento farmacológico , Pirazoles/farmacología , Analgésicos/química , Animales , Antiinflamatorios/química , Permeabilidad Capilar/efectos de los fármacos , Carragenina/toxicidad , Catecoles/química , Movimiento Celular/efectos de los fármacos , Evaluación Preclínica de Medicamentos , Leucocitos/metabolismo , Leucocitos/patología , Masculino , Ratones , Inhibidores de Fosfolipasa A2 , Fosfolipasas A2/metabolismo , Pleuresia/inducido químicamente , Pleuresia/metabolismo , Pleuresia/patología , Pirazoles/química , Factor de Necrosis Tumoral alfa/metabolismo
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